HRP20160119T1 - Inhibitor benzodiazepinske bromodomene - Google Patents

Inhibitor benzodiazepinske bromodomene Download PDF

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Publication number
HRP20160119T1
HRP20160119T1 HRP20160119TT HRP20160119T HRP20160119T1 HR P20160119 T1 HRP20160119 T1 HR P20160119T1 HR P20160119T T HRP20160119T T HR P20160119TT HR P20160119 T HRP20160119 T HR P20160119T HR P20160119 T1 HRP20160119 T1 HR P20160119T1
Authority
HR
Croatia
Prior art keywords
benzodiazepine
bromodomain inhibitor
ethylacetamide
methyloxy
triazolo
Prior art date
Application number
HRP20160119TT
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English (en)
Inventor
Romain Luc Marie Gosmini
Olivier Mirguet
Original Assignee
Glaxosmithkline Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42667965&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20160119(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB0919433A external-priority patent/GB0919433D0/en
Priority claimed from GBGB1010509.6A external-priority patent/GB201010509D0/en
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of HRP20160119T1 publication Critical patent/HRP20160119T1/hr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (3)

1. Spoj, naznačen time što je sol 2-[(4S)-6-(4-klorfenil)-1-metil-8-(metiloksi)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-il]-N-etilacetamida s benzensulfonskom kiselinom.
2. Farmaceutski pripravak, naznačen time što sadrži sol 2-[(4S)-6-(4-klorfenil)-1-metil-8-(metiloksi)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-il]-N-etilacetamida s benzensulfonskom kiselinom, kao i jednu ili više farmaceutski prihvatljivih podloga, razrjeđivača ili pomoćnih tvari.
3. Sol 2-[(4S)-6-(4-klorfenil)-1-metil-8-(metiloksi)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-il]-N-etilacetamida s benzensulfonskom kiselinom, naznačena time što je namijenjena upotrebi u terapiji.
HRP20160119TT 2009-11-05 2016-02-03 Inhibitor benzodiazepinske bromodomene HRP20160119T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0919433A GB0919433D0 (en) 2009-11-05 2009-11-05 Novel compounds
GBGB1010509.6A GB201010509D0 (en) 2010-06-22 2010-06-22 Novel compounds
EP13192666.9A EP2722334B1 (en) 2009-11-05 2010-08-06 Benzodiazepine bromodomain inhibitor

Publications (1)

Publication Number Publication Date
HRP20160119T1 true HRP20160119T1 (hr) 2016-02-26

Family

ID=42667965

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20140107AT HRP20140107T1 (hr) 2009-11-05 2014-02-05 Benzodiazepinski inhibitori bromodomene
HRP20160119TT HRP20160119T1 (hr) 2009-11-05 2016-02-03 Inhibitor benzodiazepinske bromodomene

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HRP20140107AT HRP20140107T1 (hr) 2009-11-05 2014-02-05 Benzodiazepinski inhibitori bromodomene

Country Status (32)

Country Link
US (3) US9023842B2 (hr)
EP (3) EP2722334B1 (hr)
JP (1) JP5524343B2 (hr)
KR (1) KR101424989B1 (hr)
CN (1) CN102762569B (hr)
AU (1) AU2010314395B2 (hr)
BR (1) BR112012010706A2 (hr)
CA (1) CA2779355C (hr)
CL (1) CL2012001178A1 (hr)
CO (1) CO6540003A2 (hr)
CR (1) CR20120283A (hr)
CY (2) CY1114988T1 (hr)
DK (2) DK2496580T3 (hr)
DO (1) DOP2012000114A (hr)
EA (1) EA020390B1 (hr)
ES (3) ES2652304T3 (hr)
HK (3) HK1191012A1 (hr)
HR (2) HRP20140107T1 (hr)
HU (1) HUE026421T2 (hr)
IL (2) IL219090A0 (hr)
MA (1) MA33803B1 (hr)
ME (1) ME02360B (hr)
MX (1) MX2012005295A (hr)
MY (1) MY160456A (hr)
NZ (1) NZ599258A (hr)
PE (1) PE20121181A1 (hr)
PL (2) PL2496580T3 (hr)
PT (2) PT2496580E (hr)
RS (2) RS53179B (hr)
SI (2) SI2496580T1 (hr)
SM (2) SMT201400024B (hr)
WO (1) WO2011054553A1 (hr)

Families Citing this family (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102781943B (zh) * 2009-11-05 2016-10-05 葛兰素史密丝克莱恩有限责任公司 苯并二氮杂*溴结构域抑制剂
GB0919432D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
JP6022442B2 (ja) 2010-05-14 2016-11-09 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド 男性用避妊組成物および使用方法
MX354217B (es) 2010-05-14 2018-02-19 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
AU2011252808B2 (en) 2010-05-14 2015-05-14 Dana-Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
DE102011082013A1 (de) * 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
AU2012382373A1 (en) 2012-06-12 2014-12-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
RU2015102772A (ru) * 2012-08-16 2016-10-10 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазелипы для мелкоклеточного рака легкого
PE20150729A1 (es) 2012-08-16 2015-06-14 Bayer Pharma AG 2,3-benzodiazepines
CA2886125A1 (en) 2012-09-28 2014-04-03 Bayer Pharma Aktiengesellschaft Bet protein-inhibiting 5-aryl triazole azepines
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
US9266891B2 (en) 2012-11-16 2016-02-23 Boehringer Ingelheim International Gmbh Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors
WO2014080290A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
CN105073744B (zh) 2012-12-21 2019-11-08 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新型杂环化合物
US9492460B2 (en) * 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
JP2016510039A (ja) * 2013-02-28 2016-04-04 ワシントン・ユニバーシティＷａｓｈｉｎｇｔｏｎ Ｕｎｉｖｅｒｓｉｔｙ ブロモドメイン阻害剤によるヒトサイトメガロウイルス感染および疾患の治療方法
EP2970262A1 (en) 2013-03-11 2016-01-20 AbbVie Inc. Bromodomain inhibitors
TW201444843A (zh) 2013-03-11 2014-12-01 Abbvie Inc 溴區結構域蛋白抑制劑
EA201591746A1 (ru) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
JP6280573B2 (ja) * 2013-03-14 2018-02-14 グラクソスミスクライン、インテレクチュアル、プロパティー、（ナンバー２）、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ （Ｎｏ．２） Ｌｉｍｉｔｅｄ ブロモドメイン阻害薬としてのフロピリジン
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
EP2792355A1 (en) 2013-04-17 2014-10-22 Albert-Ludwigs-Universität Freiburg Compounds for use as bromodomain inhibitors
BR112015027130A2 (pt) 2013-04-26 2018-07-24 Beigene Ltd 5-(3,5-dimetilisoxazol-4-il)indolin-2-ona substituído
CA2915561C (en) 2013-06-21 2020-09-22 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015002754A2 (en) 2013-06-21 2015-01-08 Zenith Epigenetics Corp. Novel bicyclic bromodomain inhibitors
AR096758A1 (es) * 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
ES2635560T3 (es) 2013-07-08 2017-10-04 Incyte Holdings Corporation Heterociclos tricíclicos como inhibidores de la proteína NET
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
CN105593224B (zh) 2013-07-31 2021-05-25 恒元生物医药科技(苏州)有限公司 作为溴结构域抑制剂的新型喹唑啉酮类化合物
US9428513B2 (en) 2013-11-07 2016-08-30 Boehringer Ingelheim International Gmbh Triazolopyrazine
US11446309B2 (en) 2013-11-08 2022-09-20 Dana-Farber Cancer Institute, Inc. Combination therapy for cancer using bromodomain and extra-terminal (BET) protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
GB201320994D0 (en) * 2013-11-28 2014-01-15 Univ Dundee Enzyme function probes
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
KR20160115953A (ko) 2014-01-31 2016-10-06 다나-파버 캔서 인스티튜트 인크. 디아미노피리미딘 벤젠술폰 유도체 및 그의 용도
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
CN105940005A (zh) 2014-01-31 2016-09-14 达纳-法伯癌症研究所股份有限公司 二氮杂环庚烷衍生物及其用途
JP6526060B2 (ja) 2014-02-10 2019-06-05 コンサート ファーマシューティカルズ インコーポレイテッド 置換トリアゾロベンゾジアゼピン
EP3104845A4 (en) * 2014-02-10 2017-09-27 Salk Institute for Biological Studies Increasing storage of vitamin a, vitamin d and/or lipids
WO2015121230A1 (de) * 2014-02-14 2015-08-20 Bayer Pharma Aktiengesellschaft 9-substituierte 2,3-benzodiazepine
RU2722179C2 (ru) 2014-02-28 2020-05-28 Тэнша Терапеутикс, Инк. Лечение состояний, ассоциированных с гиперинсулинемией
WO2015156601A1 (en) 2014-04-09 2015-10-15 Kainos Medicine, Inc. Bromodomain-inhibiting compounds and pharmaceutical composition comprising same for preventing or treating a cancer
NZ763737A (en) 2014-04-23 2023-04-28 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
JP6682522B2 (ja) 2014-06-20 2020-04-15 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． ２−（（４ｓ）−６−（４−クロロフェニル）−１−メチル−４ｈ−ベンゾ［ｃ］イソオキサゾロ［４，５−ｅ］アゼピン−４−イル）アセトアミドの結晶形態
NO2719005T3 (hr) 2014-07-28 2018-01-20
AU2015295405B2 (en) * 2014-08-01 2020-04-09 Nuevolution A/S Compounds active towards bromodomains
MX2017001757A (es) 2014-08-08 2017-05-30 Dana Farber Cancer Inst Inc Derivados de dihidropteridinona y sus usos.
MX2017001756A (es) 2014-08-08 2017-05-30 Dana Farber Cancer Inst Inc Derivados de diazepano y sus usos.
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
RU2697393C2 (ru) * 2014-10-02 2019-08-14 ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее
EP3212654B1 (en) 2014-10-27 2020-04-08 Tensha Therapeutics, Inc. Bromodomain inhibitors
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
EP3227281A4 (en) 2014-12-01 2018-05-30 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
US10813939B2 (en) 2014-12-05 2020-10-27 H. Lee Moffitt Cancer Center And Research Institute, Inc. Bromodomain inhibitor as adjuvant in cancer immunotherapy
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
WO2016097863A1 (en) 2014-12-17 2016-06-23 Zenith Epigenetics Corp. Inhibitors of bromodomains
EP3253756B1 (en) 2015-02-03 2021-09-22 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-c]quinoline derivatives as inhibitors of bromodomain containing proteins
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
JP2018520124A (ja) 2015-06-26 2018-07-26 テンシャ セラピューティクス，インコーポレイテッド Ｎｕｔ正中線癌の治療
JP6765622B2 (ja) 2015-07-17 2020-10-07 日本光電工業株式会社 救命支援装置
RU2750164C2 (ru) 2015-09-11 2021-06-22 Дана-Фарбер Кэнсер Инститьют, Инк. Цианотиенотриазолодиазепины и пути их применения
UA123946C2 (uk) 2015-09-11 2021-06-30 Дана-Фарбер Кенсер Інстітьют, Інк. Ацетамідтієнотриазолодіазепіни й шляхи їх застосування
CN108289957A (zh) * 2015-10-02 2018-07-17 达纳-法伯癌症研究所股份有限公司 溴区结构域抑制剂和检查点阻断的组合疗法
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
WO2017091673A2 (en) 2015-11-25 2017-06-01 Dana-Farber Cancer Institute, Inc. Bivalent bromodomain inhibtors and uses thereof
MX2018012541A (es) 2016-04-15 2019-01-17 Abbvie Inc Inhibidores de bromodominios.
US10189832B2 (en) 2016-06-20 2019-01-29 Incyte Corporation Crystalline solid forms of a BET inhibitor
WO2018022802A1 (en) 2016-07-26 2018-02-01 University Of Southern California Selective bromodomain inhibition of fungal bdf1
US20190284192A1 (en) 2016-11-10 2019-09-19 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Nitrogenous macrocyclic compound, preparation method therefor, pharmaceutical composition and application thereof
WO2019055579A1 (en) 2017-09-12 2019-03-21 Tolero Pharmaceuticals, Inc. TREATMENT REGIME FOR CANCERS THAT ARE INSENSITIVE TO BCL-2 INHIBITORS USING THE MCL-1 ALVOCIDIB INHIBITOR
CN107759607B (zh) * 2017-11-29 2019-08-23 上海万巷制药有限公司 具有抗肿瘤活性的三氮唑并二氮卓化合物及其制备方法
MX2021006544A (es) 2018-12-04 2021-07-07 Sumitomo Pharma Oncology Inc Inhibidores de cinasa dependiente de ciclina 9 (cdk9) y polimorfos de los mismos para uso como agentes para el tratamiento de cancer.
US11793802B2 (en) 2019-03-20 2023-10-24 Sumitomo Pharma Oncology, Inc. Treatment of acute myeloid leukemia (AML) with venetoclax failure
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
TW202219056A (zh) 2020-06-23 2022-05-16 美商建南德克公司 巨環化合物及其使用方法
GB202016977D0 (en) 2020-10-26 2020-12-09 In4Derm Ltd Compounds
US20230357240A1 (en) 2020-12-01 2023-11-09 Chengdu Easton Biopharmaceuticals Co., Ltd. Novel n-heterocyclic bet bromodomain inhibitor, and preparation method thereof and medical use thereof
CA3224302A1 (en) 2021-06-29 2023-01-05 Tay Therapeutics Limited Pyrrolopyridone derivatives useful in the treatment of cancer
WO2023205251A1 (en) 2022-04-19 2023-10-26 Nuevolution A/S Compounds active towards bromodomains
WO2024018423A1 (en) 2022-07-21 2024-01-25 Tay Therapeutics Limited Pyrroles and imidazoles as bet protein inhibitors

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3610848A1 (de) * 1986-04-01 1987-10-15 Boehringer Ingelheim Kg Neue 1,4-diazepine
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
CA2120939A1 (en) 1991-10-11 1993-04-15 Tetsuya Tahara Therapeutic agent for osteoporosis and diazepine compound
JPH06128257A (ja) 1992-10-13 1994-05-10 Yoshitomi Pharmaceut Ind Ltd ピリドジアゼピン化合物
JP2840454B2 (ja) 1993-11-22 1998-12-24 メルク エンド カンパニー インコーポレーテッド ベンゾジアゼピン類
IT1285567B1 (it) 1996-02-21 1998-06-18 Alfa Chem Ital Nuovo processo per la sintesi del nabumetone
IL127516A0 (en) * 1996-06-12 1999-10-28 Japan Tobacco Inc A cytokine production inhibitor
WO1998011111A1 (fr) 1996-09-13 1998-03-19 Yoshitomi Pharmaceutical Industries, Ltd. Composes de thienotriazolodiazepine et leurs utilisations a des fins medicinales
JPH11228576A (ja) * 1997-12-10 1999-08-24 Japan Tobacco Inc アポトーシス抑制剤
JP4641526B2 (ja) 2003-11-03 2011-03-02 グラクソ グループ リミテッド 流体分配デバイス
SG115845A1 (en) 2004-03-31 2005-10-28 Univ Singapore Modulation of trip-br function and method of treating proliferative disorders
GB0420970D0 (en) 2004-09-21 2004-10-20 Smithkline Beecham Corp Novel triazoloquinoline compounds
WO2006129623A1 (ja) 2005-05-30 2006-12-07 Mitsubishi Tanabe Pharma Corporation チエノトリアゾロジアゼピン化合物及びその医薬としての用途
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Ｂｒｄ２ブロモドメイン結合剤
CN101910182B (zh) 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds

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